Fazaeli Yousef, Feizi Shahzad, Jalilian Amir R, Hejrani Ali
Radiation Application Research School, Nuclear Science and Technology Research Institute (NSTRI), Moazzen Blvd., Rajaeeshahr, P.O. Box 31485-498, Karaj, Iran.
Radiation Application Research School, Nuclear Science and Technology Research Institute (NSTRI), Moazzen Blvd., Rajaeeshahr, P.O. Box 31485-498, Karaj, Iran.
Appl Radiat Isot. 2016 Jun;112:13-9. doi: 10.1016/j.apradiso.2016.03.003. Epub 2016 Mar 4.
Mesoporous silica, MCM-41, functionalized with 3-aminopropyltriethoxysilane (APTES) was investigated as a potential drug delivery system, using [(64)Cu]-5, 10, 15, 20-tetrakis penta fluorophenyl porphyrin complex. [(64)Cu]-TPPF20 complex was grafted on functionalized MCM-41. The product was characterized by paper chromatography, FTIR spectroscopy, low angle X-ray diffraction, CHN and TGA/DTA analyses and atomic force microscopy. The biological evaluations of the grafted complex, [(64)Cu]-TPPF20@NH2-MCM-41, were done in Fibrosarcoma tumor-bearing Sprague-Dawley rats using scarification studies and Sopha DST-XL Dual-Head SPECT system. The actual loading amount of aminopropyl groups was found about 1.6mmol per gram of final silica. The specific activity of the final compound was found to be 3Ci/g. Amine functionalized MCM-41 was found to be a good platform for theranostic radiopharmaceuticals such as copper-64 complexes. Considering the accumulation of the tracer in tumor cells, fast wash-out from normal tissues, the short half-life copper-64 and less imposed radiation doses to patients, [(64)Cu]-TPPF20@NH2-MCM-41 can potentially be a suitable candidate for tumor imaging applications and future PET studies.
研究了用3-氨丙基三乙氧基硅烷(APTES)功能化的介孔二氧化硅MCM-41作为潜在的药物递送系统,使用[(64)Cu]-5,10,15,20-四(五氟苯基)卟啉配合物。将[(64)Cu]-TPPF20配合物接枝到功能化的MCM-41上。通过纸色谱法、傅里叶变换红外光谱法、低角度X射线衍射、CHN和热重/差热分析以及原子力显微镜对产物进行了表征。使用划痕研究和Sopha DST-XL双头单光子发射计算机断层扫描系统,在患有纤维肉瘤的Sprague-Dawley大鼠中对接枝的配合物[(64)Cu]-TPPF20@NH2-MCM-41进行了生物学评估。发现氨丙基的实际负载量约为每克最终二氧化硅1.6mmol。发现最终化合物的比活度为3Ci/g。发现胺功能化的MCM-41是用于治疗诊断放射性药物(如铜-64配合物)的良好平台。考虑到示踪剂在肿瘤细胞中的积累、从正常组织中的快速洗脱、铜-64的短半衰期以及对患者施加的辐射剂量较小,[(64)Cu]-TPPF20@NH2-MCM-41可能是肿瘤成像应用和未来正电子发射断层扫描研究的合适候选者。